Global Patent Index - EP 2671875 A1

EP 2671875 A1 20131211 - 1-aryl-3-aminoalkoxy pyrazoles as sigma ligands enhancing analgesic effect of opioids and attenuating the dependency thereof

Title (en)

1-aryl-3-aminoalkoxy pyrazoles as sigma ligands enhancing analgesic effect of opioids and attenuating the dependency thereof

Title (de)

1-Aryl-3-Amino-alkoxy-pyrazole als Sigma-Liganden zur Verstärkung der schmerzstillenden Wirkung von Opioiden und zur Schwächung der Abhängigkeit davon

Title (fr)

Pyrazoles 1-aryl-3-aminoalkoxy utilisés comme ligands des récepteurs sigma augmentant l'effet analgésique d'opioïdes et atténuant la dépendance associée

Publication

EP 2671875 A1 20131211 (EN)

Application

EP 13176926 A 20090424

Priority

  • EP 08380122 A 20080425
  • EP 09735235 A 20090424
  • EP 13176926 A 20090424

Abstract (en)

The invention relates to the use of a group of sigma receptor ligands of formula (I) for the potentiation of the analgesic effect of opioids and opiates and at the same time for decreasing the dependency induced by them.

IPC 8 full level

A61K 31/4152 (2006.01); A61K 31/4155 (2006.01); A61K 31/485 (2006.01); A61K 45/06 (2006.01); A61P 29/00 (2006.01); C07D 231/22 (2006.01); C07D 231/26 (2006.01); C07D 401/12 (2006.01); C07D 403/12 (2006.01); C07D 471/04 (2006.01)

CPC (source: EP US)

A61K 31/4152 (2013.01 - EP US); A61K 31/4155 (2013.01 - EP US); A61K 31/485 (2013.01 - EP US); A61K 31/5377 (2013.01 - EP US); A61K 45/06 (2013.01 - EP US); A61P 25/04 (2017.12 - EP); A61P 25/36 (2017.12 - EP); A61P 29/00 (2017.12 - EP); A61P 43/00 (2017.12 - EP); C07D 231/22 (2013.01 - EP US); C07D 401/12 (2013.01 - EP US); C07D 403/12 (2013.01 - EP US); C07D 471/04 (2013.01 - EP US)

Citation (applicant)

  • EP 1130018 A1 20010905 - SANTEN PHARMACEUTICAL CO LTD [JP]
  • WO 2006021462 A1 20060302 - ESTEVE LABOR DR [ES], et al
  • EP 0975648 A1 20000202 - SALFORD ULTRAFINE CHEM & RES [GB]
  • EP 0793364 A2 19970903 - THOMSON CONSUMER ELECTRONICS [US]
  • CHICHENKOV, O. N. ET AL.: "Effect of haloperidol on the analgesic activity of intracisternally and intrathecally injected opiate agonists", FARMAKOLOGIYA I TOKSIKOLOGIYA (MOSCOW, vol. 48, no. 4, 1985, pages 58 - 61
  • "Selective antagonism of opioid analgesia by a sigma system", J PHARMACOL EXP THER, vol. 271, 1994, pages 1583 - 1590
  • "Sigma antagonists potentiate opioid analgesia in rats", NEUROSCI LETT, vol. 190, 1995, pages 137 - 139
  • MEI J. ET AL.: "confirmed the importance of sigma-1 receptors as a modulatory system on the analgesic activity of opioid drugs [Sigmal receptor modulation of opioid analgesia in the mouse", J PHARMACOL EXP THER, vol. 300, no. 3, 2002, pages 1070 - 1074
  • NOMURA, M. ET AL.: "Studies on drug dependence (Rept. 322): Attenuation of morphine- and psychostimulants-induced place preference by sigma1 receptor agonist SA4503", 72ND ANNUAL MEETING OF THE JAPANESE PHARMACOLOGICAL SOCIETY, March 1999 (1999-03-01)
  • NODA, Y. ET AL.: "A neuroactive steroid, dehydroepiandrosterone sulfate, attenuates the development of morphine dependence: an association with sigma1 receptors", 31ST ANNUAL MEETING OF THE SOCIETY OF NEUROSCIENCE, November 2001 (2001-11-01)
  • BURGER: "Medicinal Chemistry and Drug Discovery", 2001, WILEY
  • "Design and Applications of Prodrugs", 1985, HARWOOD ACADEMIC PUBLISHERS
  • CARLSSON ET AL., NEUROSCI LETT., vol. 71, no. 3, 21 November 1986 (1986-11-21), pages 356 - 60
  • JANICKI ET AL., PHARMACOL BIOCHEM BEHAVE., vol. 10, no. 4, April 1979 (1979-04-01), pages 623 - 6

Citation (search report)

  • [XY] WO 2006021462 A1 20060302 - ESTEVE LABOR DR [ES], et al
  • [YD] EP 1130018 A1 20010905 - SANTEN PHARMACEUTICAL CO LTD [JP]
  • [IY] EP 1634872 A1 20060315 - ESTEVE LABOR DR [ES]
  • [IY] EP 1829875 A1 20070905 - ESTEVE LABOR DR [ES]
  • [Y] WO 9959409 A1 19991125 - MATSUMOTO RAE R [US]
  • [YD] CHIH-CHENG CHIEN; GAVRIL W. PASTERNAK: "Sigma antagonists potentiate opioid analgesia in rats", NEUROSCIENCE LETTERS, vol. 190, no. 2, 1995, pages 137 - 139, XP002498085
  • [T] JIANJING CAO ET AL: "Dual probes for dopamine transporter and s1 receptors:novel piperazinylkylbis (4'fluorophenylamine analogues as potential cocaine-abuse therapeutic agents", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 46, no. 13, 19 June 2003 (2003-06-19), pages 2589 - 2598, XP008114796, ISSN: 0022-2623, [retrieved on 20030515], DOI: 10.1021/JM030008U
  • [T] NOMURA MUTSUKO ET AL: "Studies on drug dependence (Rept. 322): Attenuation of morphine- and psychostimulants-induced place preference by sigma1 receptor agonist SA4503", JAPANESE JOURNAL OF PHARMACOLOGY, THE JAPANESE PHARMACOLOGICAL SOCIETY, KYOTO, JP, vol. 79, no. suppl. 1, 1999, pages P-411, XP009146913, ISSN: 0021-5198
  • [T] SARI IZENWASSER ET AL: "Characterization of kappa-opioid receptor binding in human insular cortex", LIFE SCIENCES, PERGAMON PRESS, OXFORD, GB, vol. 65, no. 9, 23 July 1999 (1999-07-23), pages 857 - 862, XP008126754, ISSN: 0024-3205

Designated contracting state (EPC)

AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO SE SI SK TR

Designated extension state (EPC)

AL BA RS

DOCDB simple family (publication)

EP 2116539 A1 20091111; AU 2009239968 A1 20091029; AU 2009239968 B2 20141030; BR PI0910677 A2 20200825; CA 2722345 A1 20091029; CA 2722345 C 20160802; CN 102066334 A 20110518; CN 102066334 B 20150722; CO 6410301 A2 20120330; CY 1115848 T1 20170125; DK 2276744 T3 20150112; EC SP10010634 A 20101230; EP 2276744 A1 20110126; EP 2276744 B1 20141001; EP 2671875 A1 20131211; ES 2526360 T3 20150109; HK 1155724 A1 20120525; HR P20141263 T1 20150313; IL 208865 A0 20110131; IL 208865 B 20180430; JP 2011518807 A 20110630; JP 5753076 B2 20150722; KR 101764817 B1 20170814; KR 20110011640 A 20110208; MA 32301 B1 20110502; MX 2010011673 A 20101125; MY 160800 A 20170331; NZ 588829 A 20131025; PL 2276744 T3 20150331; PT 2276744 E 20150114; RS 53717 B1 20150430; RU 2010147925 A 20120527; RU 2519060 C2 20140610; SG 190578 A1 20130628; SI 2276744 T1 20150227; UA 105900 C2 20140710; US 2011112095 A1 20110512; US 2015018354 A1 20150115; US 2019010128 A1 20190110; US 8877753 B2 20141104; US 9914705 B2 20180313; WO 2009130310 A1 20091029

DOCDB simple family (application)

EP 08380122 A 20080425; AU 2009239968 A 20090424; BR PI0910677 A 20090424; CA 2722345 A 20090424; CN 200980122591 A 20090424; CO 10148511 A 20101125; CY 141101079 T 20141223; DK 09735235 T 20090424; EC SP10010634 A 20101125; EP 09735235 A 20090424; EP 13176926 A 20090424; EP 2009054974 W 20090424; ES 09735235 T 20090424; HK 11107451 A 20110718; HR P20141263 T 20141229; IL 20886510 A 20101021; JP 2011505522 A 20090424; KR 20107026491 A 20090424; MA 33343 A 20101111; MX 2010011673 A 20090424; MY PI2010004933 A 20090424; NZ 58882909 A 20090424; PL 09735235 T 20090424; PT 09735235 T 20090424; RS P20140694 A 20090424; RU 2010147925 A 20090424; SG 2013031166 A 20090424; SI 200931101 T 20090424; UA A201014038 A 20090424; US 201414502422 A 20140930; US 201815886145 A 20180201; US 98895109 A 20090424